Method for making 2-(18F)fluoro-2-deoxy-D-glucose

Abstract

A method is provided for making 2-[ 18 F]fluoro-2- deoxy-D-glucose which employs a phase-transfer reagent, consisting of a tetraalkylammonium bicarbonate, a tetraalkylammonium carbonate, or a mixture of a tetraalkylammonium hydroxide and potassium bicarbonate.

What is claimed is: 
     
       1. A method for making [ 18  F]fluoro-2-deoxy-D-glucose which comprises, (1) contacting at a temperature of 40° C. to 100° C., 1,3,4,6-tetra-O-acetyl-2-0-trifluoromethanesulfonyl-2-deoxy-β-D-mannopyranose and [ 18  F]fluoride ion in the presence of a 60 to 95 volume % organic solvent solution of a phase-transfer reagent selected from the class consisting of a tetraalkylammonium bicarbonate, a tetraalkylammonium carbonate and a mixture of a tetraalkylammonium hydroxide and potassium bicarbonate, and   (2) effecting the substantial removal of the organic solvent, and   (3) heating the resulting mixture of (2) in the presence of an aqueous hydrogen halide until deprotection of the resulting acetylated 2-[ 18  F]fluoro-2-deoxy-D-glucose is effected, where the organic solvent of (2) is a member selected from the class consisting of acetonitrile and propionitrile.     
     
     
       2. A method in accordance with claim 1, where the phase-transfer reagent is tetraethylammonium bicarbonate. 
     
     
       3. A method in accordance with claim 1, where the phase-transfer reagent is tetrabutylammonium bicarbonate. 
     
     
       4. A method in accordance with claim 1, where the phase-transfer reagent is tetrahexylammonium bicarbonate. 
     
     
       5. A method in accordance with claim 1, where the phase-transfer reagent is a mixture of tetraalkylammonium hydroxide and potassium bicarbonate. 
     
     
       6. A method in accordance with claim 1, where the organic solvent is acetonitrile.